G-protein-coupled receptor oligomerization and its potential for drug discovery

SR George, BF O'Dowd, SP Lee - Nature reviews Drug discovery, 2002 - nature.com
G-protein-coupled receptors (GPCRs) represent by far the largest class of targets for modern
drugs. Virtually all therapeutics that are directed towards GPCRs have been designed using …

Modelling G-protein-coupled receptors for drug design

DR Flower - Biochimica et Biophysica Acta (BBA)-Reviews on …, 1999 - Elsevier
The G-protein coupled receptors form a large and diverse multi-gene superfamily with many
important physiological functions. As such, they have become important targets in …

Structural mimicry in G protein-coupled receptors: implications of the high-resolution structure of rhodopsin for structure-function analysis of rhodopsin-like receptors

JA Ballesteros, L Shi, JA Javitch - Molecular Pharmacology, 2001 - ASPET
The availability of a high-resolution structure of rhodopsin now allows us to reconsider
research attempts to understand structure-function relationships in other G protein-coupled …

G-protein-coupled receptor dimerization: modulation of receptor function

CD Rios, BA Jordan, I Gomes, LA Devi - Pharmacology & therapeutics, 2001 - Elsevier
G-protein-coupled receptors (GPCRs) comprise the largest family of transmembrane
receptors in the human genome that respond to a plethora of signals, including …

D2/D3 dopamine receptor heterodimers exhibit unique functional properties

M Scarselli, F Novi, E Schallmach, R Lin… - Journal of Biological …, 2001 - ASBMB
Evidence for heterodimerization has recently been provided for dopamine D 1 and
adenosine A 1 receptors as well as for dopamine D 2 and somatostatin SSTR 5 receptors. In …

Synthesis, CoMFA Analysis, and Receptor Docking of 3,5-Diacyl-2,4-Dialkylpyridine Derivatives as Selective A3 Adenosine Receptor Antagonists

AH Li, S Moro, N Forsyth, N Melman, X Ji… - Journal of medicinal …, 1999 - ACS Publications
3, 5-Diacyl-2, 4-dialkyl-6-phenylpyridine derivatives have been found to be selective
antagonists at both human and rat A3 adenosine receptors (Li et al. J. Med. Chem. 1998, 41 …

Evidence for adenosine/dopamine receptor interactions: indications for heteromerization

R Franco, S Ferré, L Agnati, M Torvinen, S Ginés… - …, 2000 - Elsevier
Evidence has been obtained for adenosine/dopamine interactions in the central nervous
system. There exists an anatomical basis for the existence of functional interactions between …

G protein coupled receptor dimerization: implications in modulating receptor function

I Gomes, BA Jordan, A Gupta, C Rios… - Journal of molecular …, 2001 - Springer
Protein-protein interactions are involved in the regulation of a large number of biological
processes. It is well established that a variety of cell surface receptors interact with each …

D2 dopamine receptor homodimerization is mediated by multiple sites of interaction, including an intermolecular interaction involving transmembrane domain 4

SP Lee, BF O'Dowd, RD Rajaram, T Nguyen… - Biochemistry, 2003 - ACS Publications
In this study, we examined the mechanisms of intermolecular interaction involved in D2
dopamine receptor dimer formation to develop an understanding of the quaternary structure …

Inhibition of cell surface expression by mutant receptors demonstrates that D2 dopamine receptors exist as oligomers in the cell

SP Lee, BF O'Dowd, GYK Ng, G Varghese, H Akil… - Molecular …, 2000 - ASPET
Numerous mutant G protein-coupled receptors with diminished or no function have been
described that are naturally occurring or that are the product of gene manipulation. It has …